CYCLOSPORIN-A, A PEPTIDE METABOLITE FROM TRICHODERMA-POLYSPORUM (LINK EX PERS) RIFAI, WITH A REMARKABLE IMMUNOSUPPRESSIVE ACTIVITY

被引：346

作者：

RUEGGER, A ^{[1
]}

KUHN, M ^{[1
]}

LICHTI, H ^{[1
]}

LOOSLI, HR ^{[1
]}

HUGUENIN, R ^{[1
]}

QUIQUEREZ, C ^{[1
]}

WARTBURG, AV ^{[1
]}

机构：

[1] SANDOZ AG, DEPT PHARM CHEM FORSCH, CH-4002 BASEL, SWITZERLAND

来源：

HELVETICA CHIMICA ACTA | 1976年 / 59卷 / 04期

关键词：

D O I：

10.1002/hlca.19760590412

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Two antifungal metabolites, cyclosporins A and C, were isolated from a strain of T. polysporum (Link ex Pers.) Rifai. Cyclosporin A, the main component, has the molecular formula C62H111N11O12 as deduced by NMR and mass spectra. Hydrolytic cleavage of cyclosporin A furnished 11 amino acids as fragments, among them an artefact of a new C9-amino acid. The amino acid sequence was determined by Edman degradation of iso-cyclosporin A, a basic rearrangement product formed from cyclosporin A by N,O-acyl migration. In an independent investigation an X-ray analysis of the iodo derivative was perfromed. On the basis of the chemical, spectroscopic and crystallographic evidence the complete structure of cyclosporin A was elucidated. Cyclosporin A and C show remarkable immunosuppressive and antiphlogistic activities in several pharmacological models.

引用

页码：1075 / 1092

页数：18

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